| 名稱 | ACY-775 |
| 描述 | ACY-775 is an effective and specific inhibitor of HDAC6 (IC50: 7.5 nM). |
| 細(xì)胞實(shí)驗(yàn) | Undifferentiated RN46A-B14 cells are grown. They are treated with 2.5?μM ACY-738, ACY-775, tubastatin A, 0.6?μM TSA or vehicle (0.1% DMSO) for 4?h. Samples are processed using a histone extraction kit and quantified using protein assay [2]. |
| 動物實(shí)驗(yàn) | Mice are tested for immobility in the TST. At 30?min or 2?h after i.p. injection of ACY-738 (5, 50?mg/kg), ACY-775 (5, 50?mg/kg), and citalopram (0.5, 2, 20?mg/kg), a combination of the previous, or vehicle, mice are attached to the test rig and time immobile over 6?min is recorded. For open-field activity, mice are injected with ACY-738 or ACY-775 at 5, 10, or 50?mg/kg or vehicle and allowed to explore [2]. |
| 體外活性 | Upon treatment with ACY-775, a clear enhancement of the acetylation of α-tubulin is visible, while histone acetylation remains unaltered. Acetylation of α-tubulin is visualized by immunofluorescence and the intensity in the neurites of the neurons is quantified and normalized to the length of the fluorescent signal. In vehicle-treated DRG neurons, acetylated α-tubulin is already present. Upon treatment with ACY-775, the signal intensity of acetylated α-tubulin increases significantly. A significant increase in motility of mitochondria and also the total number of mitochondria within the neurites are observed compared with vehicle-treated DRG neurons. A significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compared with vehicle-treated cells [1]. |
| 體內(nèi)活性 | Biodistribution profiles of ACY-775 are examined after acute dosing at 5 or 50?mg/kg over 2?h. At t=30?min after acute 50?mg/kg injection, respective plasma levels of ACY-775 is 1359?ng/mL (4.1?μM). Elimination from the plasma is rapid, with a plasmatic half-life of 12?min and a concentration below 10?ng/mL after 2?h. When ACY-775 (50?mg/kg) is administered repeatedly in wild-type mice at 24?h, 4?h, and 30?min before killing, significant increases in α-tubulin acetylation are observed in all tested brain regions [2]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (302.70 mM), Sonication and heating are recommended.
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| 關(guān)鍵字 | Histone deacetylases | inhibit | ACY 775 | Inhibitor | ACY775 | ACY-775 | HDAC |
| 相關(guān)產(chǎn)品 | Valproic acid sodium salt | 4-Phenylbutyric acid | Valproic Acid | Panobinostat | Methyl L-histidinate dihydrochloride | Theophylline | Acefylline | Curcumin | Theophylline monohydrate | Sodium 4-phenylbutyrate | Vorinostat | Parthenolide |
| 相關(guān)庫 | 抑制劑庫 | 抗乳腺癌化合物庫 | 經(jīng)典已知活性庫 | 抗癌化合物庫 | 已知活性化合物庫 | 抗胰腺癌化合物庫 | 抗衰老化合物庫 | 表觀遺傳庫 | NO PAINS 化合物庫 | NF-κB 通路分子庫 |